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A practical synthesis of m-prostaglandin E synthase-1 inhibitor MK-7285
Francis Gosselin1, Stephen Lau, Christian Nadeau
1Department of Process Research, Merck Frosst Centre for Therapeutic Research, 16711 Route Transcanadienne, Kirkland, Québec, Canada H9H 3L1. francis_gosselin@merck.com
Abstract:
A practical, kilogram-scale chromatography-free synthesis of mPGE synthase I inhibitor MK-7285 is described. The route features a convergent assembly of the core phenanthrene unit via amide-directed ortho-metalation and proximity-induced anionic cyclization, followed by imidazole synthesis and late-stage cyanation.
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